نتایج جستجو برای: ezh2

تعداد نتایج: 2721  

Journal: :Molecular cancer therapeutics 2014
Sarah K Knutson Satoshi Kawano Yukinori Minoshima Natalie M Warholic Kuan-Chun Huang Yonghong Xiao Tadashi Kadowaki Mai Uesugi Galina Kuznetsov Namita Kumar Tim J Wigle Christine R Klaus Christina J Allain Alejandra Raimondi Nigel J Waters Jesse J Smith Margaret Porter-Scott Richard Chesworth Mikel P Moyer Robert A Copeland Victoria M Richon Toshimitsu Uenaka Roy M Pollock Kevin W Kuntz Akira Yokoi Heike Keilhack

Mutations within the catalytic domain of the histone methyltransferase EZH2 have been identified in subsets of patients with non-Hodgkin lymphoma (NHL). These genetic alterations are hypothesized to confer an oncogenic dependency on EZH2 enzymatic activity in these cancers. We have previously reported the discovery of EPZ005678 and EPZ-6438, potent and selective S-adenosyl-methionine-competitiv...

2016
Goro Sashida Changshan Wang Takahisa Tomioka Motohiko Oshima Kazumasa Aoyama Akinori Kanai Makiko Mochizuki-Kashio Hironori Harada Kazuya Shimoda Atsushi Iwama

EZH2 is a component of polycomb repressive complex 2 (PRC2) and functions as an H3K27 methyltransferase. Loss-of-function mutations in EZH2 are associated with poorer outcomes in patients with myeloproliferative neoplasms (MPNs), particularly those with primary myelofibrosis (MF [PMF]). To determine how EZH2 insufficiency is involved in the pathogenesis of PMF, we generated mice compound for an...

2014
Anika Tschirner Sandra Palus Roland Hetzer Rudolf Meyer Stefan D. Anker Jochen Springer

BACKGROUND Recently, it was shown that a knock-out (KO) of the polycomb histone methyltransferase Ezh2 leads to cardiac hypertrophy in mice, which was driven by the homeodomain transcription factor Six1. Here, we analyzed the expression of Six1 and its regulating factor Ezh2 in cardiac tissue of patients with end-stage dilative cardiomyopathy (DCM). METHODS Tissue samples of patients with end...

Journal: :Molecular cancer therapeutics 2009
Feng Sun Eli Chan Zhenlong Wu Xiaojing Yang Victor E Marquez Qiang Yu

Polycomb protein EZH2-mediated gene silencing is implicated in breast tumorigenesis through methylation of histone H3 on Lysine 27 (H3K27). We have previously shown that S-adenosylhomocysteine hydrolase inhibitor 3-deazaneplanocin A can modulate histone methylation and disrupt EZH2 complex. Here, we used 3-deazaneplanocin A, together with other chromatin remodeling agents, as well as RNA interf...

Journal: :Molecular cancer therapeutics 2006
Warren Fiskus Michael Pranpat Maria Balasis Bryan Herger Rekha Rao Arul Chinnaiyan Peter Atadja Kapil Bhalla

Human enhancer of zeste 2 (EZH2) protein belongs to the multiprotein polycomb repressive complex 2, which also includes suppressor of zeste 12 (SUZ12) and embryonic ectoderm development (EED). The polycomb repressive complex 2 complex possesses histone methyltransferase activity mediated by the Su(var)3-9, enhancer of zeste, and trithorax domain of EZH2, which methylates histone H3 on lysine (K...

2014
Swathi Chinaranagari Pankaj Sharma Jaideep Chaudhary

Inhibitor of DNA binding/differentiation protein 4 (ID4) is dominant negative helix loop helix transcriptional regulator is epigenetically silenced due to promoter hyper-methylation in many cancers including prostate. However, the underlying mechanism involved in epigenetic silencing of ID4 is not known. Here, we demonstrate that ID4 promoter methylation is initiated by EZH2 dependent tri-methy...

2015
Tijana Mitić Andrea Caporali Ilaria Floris Marco Meloni Micol Marchetti Raul Urrutia Gianni D Angelini Costanza Emanueli

Epigenetic mechanisms may regulate the expression of pro-angiogenic genes, thus affecting reparative angiogenesis in ischemic limbs. The enhancer of zest homolog-2 (EZH2) induces thtrimethylation of lysine 27 on histone H3 (H3K27me3), which represses gene transcription. We explored (i) if EZH2 expression is regulated by hypoxia and ischemia; (ii) the impact of EZH2 on the expression of two pro-...

2015
Yang-Fan Lv Guang-Ning Yan Gang Meng Xi Zhang Qiao-Nan Guo

The enhancer of zeste homolog 2 (EZH2) methyltransferase is the catalytic subunit of polycomb repressive complex 2 (PRC2), which acts as a transcription repressor via the trimethylation of lysine 27 of histone 3 (H3K27me3). EZH2 has been recognised as an oncogene in several types of tumors; however, its role in osteosarcoma has not been fully elucidated. Herein, we show that EZH2 silencing inhi...

2014
Wei Zhang Shengqing Lv Jun Liu Zhenle Zang Junyi Yin Ning An Hui Yang Yechun Song

PCI-24781 is a novel histone deacetylase inhibitor that inhibits tumor proliferation and promotes cell apoptosis. However, it is unclear whether PCI-24781 inhibits Enhancer of Zeste 2 (EZH2) expression in malignant gliomas. In this work, three glioma cell lines were incubated with various concentrations of PCI-24781 (0, 0.25, 0.5, 1, 2.5 and 5 μM) and analyzed for cell proliferation by the MTS ...

2015
Kyung Hyun Yoo Sumin Oh Keunsoo Kang Tim Hensel Gertraud W. Robinson Lothar Hennighausen

Establishment and differentiation of mammary alveoli during pregnancy are controlled by prolactin through the transcription factors STAT5A and STAT5B (STAT5), which also regulate temporal activation of mammary signature genes. This study addressed the question whether the methyltransferase and transcriptional co-activator EZH2 controls the differentiation clock of mammary epithelium. Ablation o...

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